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Design principles for optogenetic-based targeted protein degradation [PDF]
Synthetic and Systems BiotechnologyPrecise regulation of protein abundance is essential for understanding dynamic cellular processes and for advancing therapeutic development. However, existing approaches lack the spatiotemporal resolution required to these cellular processes.
Yunyue Chen +5 more
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Targeted protein degradation: species, diseases and efficient utilization [PDF]
Journal of Translational MedicineBackground Targeted protein degradation (TPD) is a novel protein modulation strategy distinct from traditional inhibitors. Its core mechanism involves labeling proteins of interest to initiate endogenous protein clearance pathways, mainly including the ...
Tian Yue, Jian He, Jun Hou
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De novo designed protein guiding targeted protein degradation [PDF]
Nature CommunicationsTargeted protein degradation is a powerful tool for biological research, cell therapy, and synthetic biology. However, conventional methods often depend on pre-fused degrons or chemical degraders, limiting their wider applications.
Zhendong Li +10 more
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PROTAC-induced protein structural dynamics in targeted protein degradation [PDF]
eLifePROteolysis TArgeting Chimeras (PROTACs) are small molecules that induce target protein degradation via the ubiquitin-proteasome system. PROTACs recruit the target protein and E3 ligase; a critical first step is forming a ternary complex.
Kingsley Y Wu +2 more
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Targeted protein degradation in Escherichia coli using CLIPPERs [PDF]
EMBO ReportsNew, universal tools for targeted protein degradation in bacteria can help to accelerate protein function studies and antimicrobial research. We describe a new method for degrading bacterial proteins using plasmid-encoded degrader peptides which deliver ...
Matylda Anna Izert-Nowakowska +9 more
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Cellular parameters shaping pathways of targeted protein degradation [PDF]
Communications BiologyIn recent years the development of proteolysis-targeting chimeras (PROTACs) has enhanced the field of ubiquitin signalling through advancing therapeutic targeted protein degradation (TPD) strategies and generating tools to explore the ubiquitin landscape.
Annabel Cardno +2 more
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Targeted protein degradation with small molecules for cancer immunotherapy [PDF]
Asian Journal of Pharmaceutical SciencesImmunotherapy has transformed cancer treatment, marked by the approval of numerous antibody-based drugs. However, the limitations of antibodies in pharmacokinetics including long half-lives, limited oral bioavailability and immunogenicity, have prompted ...
Zichao Yang +3 more
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Targeted protein degradation by KLHDC2 ligands identified by high-throughput screening [PDF]
eLifeProteolysis-targeting chimeras (PROTACs) enable the selective and sub-stoichiometric elimination of pathological proteins, yet only two E3 ligases are routinely used for this purpose.
Han Zhou +8 more
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Gluing Proteins for Targeted Degradation [PDF]
Cancer Cell, 2021 Targeted protein degradation is an emerging technology for drug development. An article published in Nature reported a novel mechanism of targeted protein degradation triggered by small-molecule-induced polymerization of the oncogenic transcription factor BCL6.
Mikihiko, Naito, Shigeo, Murata
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Piperlongumine conjugates induce targeted protein degradation [PDF]
Cell Chemical Biology, 2022 SUMMARYPROteolysis Targeting Chimeras (PROTACs) are bifunctional molecules that degrade target proteins through recruiting E3 ligases. However, their application is limited in part because few E3 ligases can be recruited by known E3 ligase ligands. In this study, we identified piperlongumine (PL), a natural product, as a covalent E3 ligase recruiter ...
Jing Pei +16 more
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